1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

Autophagy is a conserved cellular degradation and recycling process in the lysosome. In mammalian cells, there are three primary types of autophagy: microautophagy, macroautophagy, and chaperone-mediated autophagy (CMA). Microphagy captures cargoes by means of invaginations or protrusions of the lysosomal membrane directly, CMA uses chaperones to identify cargo proteins and then unfolds and transfers them into the lysosomal, while macroautophagy sequesters cargo by autophagosomes-de novo synthesized of double-membrane vesicles-and subsequently transport it to the lysosome.

Macroautophagy is the best studied and it occurs at a low level constitutively and can also be further induced under stress conditions, such as nutrient or energy starvation with a salient feature of autophagy protein degradation. Stress-induced macrophagy plays an important role in protein catabolism with another key protein degradation pathway, the ubiquitin–proteasome system (UPS).

As the study progressed, autophagy gains its importance under basal, nutrient-rich conditions, and is now recognized as a critical housekeeping pathway in catabolism of diverse cellular constituents, such as protein aggregates (aggrephagy), lipid droplets (lipophagy), iron complex (Ferritinophagy) and carbohydrate. Except for macromolecules, autophagy can also target several organelles and structures, such as mitochondria (mitophagy), peroxisome (pexophagy), endoplasmic reticulum (reticulophagy or ER-phagy), ribosome (ribophagy), spermatozoon-inherited organelles following fertilization (allophagy), secretory granules within pancreatic cells (zymophagy) and intracellular pathogens (xenophagy).

Autophagy and its dysfunction are associated with a variety of human pathologies, including ageing, cancer, neurodegenerative disease, heart disease and metabolic diseases, such as diabetes. Plenty of drugs and natural products are involved in autophagy modulation through multiple signaling pathways. Small molecules that can regulate autophagy seem to have great potential to intervene such diseases in animal models or clinical courses.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0228S3
    Adenosine-3′-13C
    Adenosine-3′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
    Adenosine-3′-<sup>13</sup>C
  • HY-W584517
    Thalidomide-5-O-CH2-COO(t-Bu)
    Inducer
    Thalidomide-5-O-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-5-O-CH2-COO(t-Bu)
  • HY-173133
    Antitumor agent-199
    Inducer
    Antitumor agent-199 (Compound 4b) is an antitumor agent. Antitumor agent-199 exhibits significant antiproliferative activity against multiple tumor cell lines. Antitumor agent-199 can induce autophagy in cancer cells via the ATG5/ATG7 pathway and can be used in the study of cancer.
    Antitumor agent-199
  • HY-13955S2
    Telmisartan-13C,d3
    Inducer
    Telmisartan-13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
    Telmisartan-<sup>13</sup>C,d<sub>3</sub>
  • HY-A0067R
    Oxybenzone (Standard)
    Inhibitor
    Oxybenzone (Standard) is the analytical standard of Oxybenzone. This product is intended for research and analytical applications. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
    Oxybenzone (Standard)
  • HY-N2593R
    Isorhapontigenin (Standard)
    Inducer
    Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin. This product is intended for research and analytical applications. Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation.
    Isorhapontigenin (Standard)
  • HY-12033S
    2-Methoxyestradiol-13C,d3
    Inducer
    2-Methoxyestradiol-13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
    2-Methoxyestradiol-<sup>13</sup>C,d<sub>3</sub>
  • HY-N0281R
    Daphnetin (Standard)
    Inducer
    Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
    Daphnetin (Standard)
  • HY-10572S1
    Efavirenz-13C6
    Inducer
    Efavirenz-13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
    Efavirenz-<sup>13</sup>C<sub>6</sub>
  • HY-N0013R
    Vitexin (Standard)
    Vitexin (Standard) is the analytical standard of Vitexin. This product is intended for research and analytical applications. Vitexin is a c-glycosylated flavone, and is found in various medicinal plants species such as Trigonella foenum-graecum Linn. Vitexin has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.
    Vitexin (Standard)
  • HY-B1287R
    Citalopram (hydrobromide) (Standard)
    Inducer
    Citalopram (hydrobromide) (Standard) is the analytical standard of Citalopram (hydrobromide). This product is intended for research and analytical applications. Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
    Citalopram (hydrobromide) (Standard)
  • HY-148255
    QN523
    Inducer 99.77%
    QN523 is a novel scaffold with agent-like properties, showing potent in vitro cytotoxicity in a panel of 12 cancer cell lines. QN523 induces apoptosis and autophagy. QN523 can be used in research of cancer.
    QN523
  • HY-163193
    MJO445
    MJO445 (Compound 7) is a ATG4B inhibitor, which inhibits the autophagy of glioblastoma.
    MJO445
  • HY-156187
    Anticancer agent 161
    Anticancer agent 161 (Compound 3b) is a bioactive alkynol with anti-cancer potential. Anticancer agent 161 can trigger autophagy and mitochondrial membrane potential depletion.
    Anticancer agent 161
  • HY-N0087R
    Gambogic Acid (Standard)
    Inducer
    Gambogic Acid (Standard) is the analytical standard of Gambogic Acid. This product is intended for research and analytical applications. Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
    Gambogic Acid (Standard)
  • HY-138849
    Thalidomide-NH-amido-C2-NH2
    Inducer
    Thalidomide-NH-amido-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C2-NH2
  • HY-N1462R
    Atractyloside (potassium salt) (Standard)
    Activator
    Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity.
    Atractyloside (potassium salt) (Standard)
  • HY-N2117R
    Isoginkgetin (Standard)
    Activator
    Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.
    Isoginkgetin (Standard)
  • HY-B0233S2
    Isradipine-d7
    Inducer
    Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.
    Isradipine-d<sub>7</sub>
  • HY-10999S2
    Trametinib-13C,d3
    Inducer
    Trametinib-13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
    Trametinib-<sup>13</sup>C,d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity